 | Tofacitinib | IC50 | 34.0 [1] |
| Tofacitinib | Ki | 4.39 [1], 7.3 [2], 7.8 [3] |
 | Ruxolitinib | IC50 | 19.0 [1] |
| Ruxolitinib | Ki | 0.5 [1], 0.55 [2] |
 | Pyridone 6 | IC50 | 1.0 [1], 5.0 [2], 1700.0 [3] |
 | Baricitinib | IC50 | 8.7 [1], 53.0 [2], 61.0 [3], 200000.0 [4] |
 | Filgotinib | IC50 | 86.77 [1], 116.0 [2], 2600.0 [3] |
 | N-[(1R)-1-[3-[12-Methyl-8-(methylamino)-5-thia-3,7,10,12-tetrazatricyclo[7.3.0.02,6]dodeca-1(9),2(6),3,7,10-pentaen-4-yl]phenyl]ethyl]-2-methylsulfonylbenzamide | IC50 | 27.0 [1], 970.0 [2], 1000.0 [3], 2000.0 [4] |
 | 6-Anilino-8-(cyclopropylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 32.0 [1], 1100.0 [2], 1500.0 [3], 2000.0 [4] |
 | 6-(Cyclohexylamino)-8-(cyclopropylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 220.0 [1], 2000.0 [2], 3200.0 [3], 3400.0 [4] |
 | 6-(3,5-Difluoro-2-methoxyanilino)-N-[(2S)-2,3-dihydroxy-2-methylpropyl]-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 4.0 [1], 160.0 [2], 240.0 [3], 370.0 [4] |
 | 8-[[(2R)-2,3-Dihydroxy-2-methylpropyl]amino]-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]anilino]imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 8.0 [1], 750.0 [2], 780.0 [3], 4200.0 [4] |
 | 6-[3-Cyano-5-(trifluoromethyl)anilino]-8-(cyclopropylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 480.0 [1], 8200.0 [2], 12600.0 [3], 50000.0 [4] |
 | 8-[[(1S,2R)-2-Fluorocyclopropyl]amino]-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]anilino]imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 25.0 [1], 320.0 [2], 410.0 [3], 10000.0 [4] |
 | 8-(Cyclopropylamino)-6-(3-fluoro-5-methylanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 24.0 [1], 1400.0 [2], 1700.0 [3], 2000.0 [4] |
 | 8-(Cyclopropylamino)-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 22.0 [1], 700.0 [2], 1400.0 [3], 50000.0 [4] |
 | N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide | IC50 | 1250.0 [1], 200000.0 [2] |
 | 2,6-Dichloro-N-{2-[(Cyclopropylcarbonyl)amino]pyridin-4-Yl}benzamide | Ki | 4.8 [1] |
 | 3-[5-[4-(2-Hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione | IC50 | 1691.0 [1], 2110.0 [2], 8055.0 [3] |
 | 1-(2-Aminoethyl)-2-(4-piperidinyl)-1H-benzoimidazole-5-carboxamide | IC50 | 3700.0 [1], 759500.0 [2] |
 | 1-Cyclopropyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]methanesulfonamide | IC50 | 1870.0 [1], 10000.0 [2], 200000.0 [3] |
 | Tyk2-IN-2 | IC50 | 7.0 [1], 50.0 [2], 100.0 [3] |
 | 4-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]benzonitrile | IC50 | 56.0 [1], 140.0 [2], 370.0 [3] |
 | 4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)-N-(2-phenylethyl)cyclohexan-1-amine | IC50 | 180.0 [1], 230.0 [2], 1000.0 [3] |
 | 4-Fluoro-N-[4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]aniline | IC50 | 130.0 [1], 240.0 [2], 1000.0 [3] |
 | 8-(Cyclobutylamino)-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 110.0 [1], 4100.0 [2], 6200.0 [3] |
 | 6-(3,5-Dimethylanilino)-8-(ethylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 17.0 [1], 600.0 [2] |
 | 8-Anilino-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 50.0 [1], 3700.0 [2], 4900.0 [3] |
 | 8-(Methylamino)-6-(3-phenylanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 4.0 [1], 200.0 [2], 330.0 [3] |
 | 8-(Cyclopropylamino)-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]anilino]imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 66.0 [1], 1100.0 [2], 1200.0 [3] |
 | 6-(3,5-Dimethylanilino)-N-[3-hydroxy-2-(hydroxymethyl)-2-methylpropyl]-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 15.0 [1], 330.0 [2], 480.0 [3] |
 | 6-(3-Tert-butylanilino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 13.0 [1], 410.0 [2], 510.0 [3] |
 | N-[(2S)-2,3-Dihydroxy-2-methylpropyl]-8-(methylamino)-6-(2,3,5,6-tetrafluoroanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 8.0 [1], 300.0 [2], 450.0 [3] |
 | 6-(3,5-Dimethylanilino)-N-(3-hydroxy-2,2-dimethylpropyl)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 2.0 [1], 110.0 [2], 300.0 [3] |
 | N-Cyclopropyl-6-(3,5-dimethylanilino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 8.0 [1], 100.0 [2], 110.0 [3] |
 | 8-(Cyclopentylamino)-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 500.0 [1], 4800.0 [2], 7300.0 [3] |
 | 6-(3,5-Difluoro-2-methoxyanilino)-N-(3-hydroxy-2,2-dimethylpropyl)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 6.0 [1], 30.0 [2], 70.0 [3] |
 | N-Cyclopropyl-6-(2,3-dihydro-1,4-benzodioxin-5-ylamino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 6.0 [1], 10.0 [2], 20.0 [3] |
 | N-(3-Hydroxy-2,2-dimethylpropyl)-6-(2-methoxyanilino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamide | IC50 | 5.0 [1], 120.0 [2], 150.0 [3] |
 | Staurosporine | IC50 | 0.35 [1], 0.6 [2] |
 | Oclacitinib | IC50 | 75.1 [1] |
 | Decernotinib | IC50 | 11.0 [1], 10000.0 [2] |
 | 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one | IC50 | 10000.0 [1] |
 | 2-Chloro-4-cyano-6-fluoro-N-[2-[[(1R,2R)-2-fluorocyclopropanecarbonyl]amino]pyridin-4-yl]benzamide | Ki | 1.6 [1] |
 | 4-Amino-N-methyl-2-phenylthieno[3,2-c]pyridine-7-carboxamide | IC50 | 937.0 [1], 25000.0 [2] |
 | 3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-(1-methyl-5-morpholin-4-ylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 0.55 [1], 200.0 [2] |
 | 3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-(5-morpholin-4-ylpyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 0.92 [1], 48.0 [2] |
 | 3-Amino-5-(2-methylpropyl)-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 72.0 [1], 1100.0 [2] |
 | 3-Amino-5-[(2R)-3-methylbutan-2-yl]-7-(5-morpholin-4-ylpyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 9.7 [1], 440.0 [2] |
 | 3-Amino-5-(3-methylbutan-2-yl)-7-(5-morpholin-4-ylpyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 1.5 [1], 54.0 [2] |
 | 3-Amino-5-(3-methylbutan-2-yl)-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 6.3 [1], 310.0 [2] |
 | 3-Amino-5-(2-methylpentan-3-yl)-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 91.0 [1], 6900.0 [2] |
 | 3-Amino-7-[5-(2-hydroxypropan-2-yl)-1-methylpyrazol-3-yl]-5-[(2R)-3-methylbutan-2-yl]-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 2.1 [1], 190.0 [2] |
 | 3-Amino-7-[5-(1,1-dioxo-1,4-thiazinan-4-yl)-1-methylpyrazol-3-yl]-5-[(2S)-3-methylbutan-2-yl]-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 1.2 [1], 230.0 [2] |
 | 3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-[1-methyl-5-(oxan-4-yl)pyrazol-3-yl]-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 0.98 [1], 110.0 [2] |
 | 2-Cyano-3-[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]-N,N-dimethylprop-2-enamide | IC50 | 459.0 [1], 11800.0 [2] |
 | 4-Amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 66.0 [1], 25000.0 [2] |
 | 4-Amino-N-Methyl-2-[4-(Morpholin-4-Yl)phenyl]thieno[3,2-C]pyridine-7-Carboxamide | IC50 | 1330.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(Tert-Butylsulfamoyl)phenyl]-N-Methylthieno[3,2-C]pyridine-7-Carboxamide | IC50 | 266.0 [1], 25000.0 [2] |
 | Infigratinib phosphate | IC50 | 3303.0 [1], 10000.0 [2] |
 | 4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-[2-(dimethylamino)ethyl]thieno[3,2-c]pyridine-7-carboxamide | IC50 | 4100.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-morpholin-4-ylethyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 757.0 [1], 25000.0 [2] |
 | 4-Amino-N-methyl-2-(4-methylphenyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 888.0 [1], 25000.0 [2] |
 | 4-Amino-2-(4-tert-butylphenyl)-N-methylthieno[3,2-c]pyridine-7-carboxamide | IC50 | 202.0 [1], 25000.0 [2] |
 | 4-Amino-N-methyl-2-[4-(trifluoromethoxy)phenyl]thieno[3,2-c]pyridine-7-carboxamide | IC50 | 208.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(2-cyanopropan-2-yl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamide | IC50 | 146.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-hydroxyethyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 932.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-methoxyethyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 1480.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-piperidin-1-ylethyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 2670.0 [1], 25000.0 [2] |
 | 4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(3-morpholin-4-ylpropyl)thieno[3,2-c]pyridine-7-carboxamide | IC50 | 1550.0 [1], 25000.0 [2] |
 | N-[2-(2,6-Dichlorophenyl)-[1,3]thiazolo[5,4-c]pyridin-4-yl]cyclopropanecarboxamide | Ki | 0.5 [1] |
 | N-Methyl-N-[3-(propylsulfonylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine | IC50 | 3610.0 [1], 200000.0 [2] |
 | N-[3-(Butylsulfonylmethyl)cyclobutyl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine | IC50 | 553.0 [1], 200000.0 [2] |
 | 2,2,2-Trifluoro-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]ethanesulfonamide | IC50 | 1020.0 [1], 200000.0 [2] |
 | 2-Methyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]propane-1-sulfonamide | IC50 | 479.0 [1], 200000.0 [2] |
 | N-[3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]-1-(oxetan-3-yl)methanesulfonamide | IC50 | 2380.0 [1], 200000.0 [2] |
 | 3-N-(Cyclopropylmethylsulfamoyl)-1-N-methyl-1-N-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)cyclobutane-1,3-diamine | IC50 | 1780.0 [1], 200000.0 [2] |
 | 4-[[3-[[2-Cyanoethyl(methyl)sulfamoyl]amino]cyclobutyl]-methylamino]-7H-pyrrolo[2,3-d]pyrimidine | IC50 | 1190.0 [1], 200000.0 [2] |
 | 3-Amino-5-butan-2-yl-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 33.0 [1], 650.0 [2] |
 | 3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-one | IC50 | 5.5 [1], 150.0 [2] |
 | 2-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]acetonitrile | IC50 | 2.9 [1], 170.0 [2] |
 | 4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-ol | IC50 | 96.0 [1], 150.0 [2] |
 | [4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methanol | IC50 | 38.0 [1], 150.0 [2] |
 | 1-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]azetidin-3-ol | IC50 | 49.0 [1], 810.0 [2] |
 | 4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexane-1-carbaldehyde | IC50 | 55.0 [1], 100.0 [2] |
 | 2-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]propanenitrile | IC50 | 25.0 [1], 1000.0 [2] |
 | (3R)-1-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]pyrrolidin-3-ol | IC50 | 19.0 [1], 770.0 [2] |
 | N-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]morpholin-4-amine | IC50 | 500.0 [1], 1000.0 [2] |
 | 2-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]-N-(2,2,2-trifluoroethyl)acetamide | IC50 | 1000.0 [1] |
 | N-(2-Bromo-2,2-difluoroethyl)-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amine | IC50 | 13.0 [1], 760.0 [2] |
 | N-[(4-Chlorophenyl)methyl]-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amine | IC50 | 110.0 [1], 150.0 [2] |
 | 1,1,1-Trifluoro-3-[[4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]-2-phenylpropan-2-ol | IC50 | 270.0 [1], 1000.0 [2] |
 | N-[(4-Fluorophenyl)methyl]-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amine | IC50 | 120.0 [1], 310.0 [2] |
 | (3S)-1-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]pyrrolidin-3-ol | IC50 | 100.0 [1], 1000.0 [2] |
 | N-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]cyclopropanamine | IC50 | 100.0 [1], 940.0 [2] |
 | N-Benzyl-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amine | IC50 | 110.0 [1], 330.0 [2] |
 | 2-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]-N-(2,2,2-trifluoroethyl)acetamide | IC50 | 790.0 [1], 880.0 [2] |
 | N-(Cyanomethyl)-2-[4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]acetamide | IC50 | 540.0 [1], 1000.0 [2] |
 | 4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)-N-(3-phenylpropyl)cyclohexan-1-amine | IC50 | 450.0 [1], 1000.0 [2] |
 | 4-[[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]methyl]benzonitrile | IC50 | 88.0 [1], 310.0 [2] |
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